92534-73-1Relevant academic research and scientific papers
DNA POLYMERASE IIIC INHIBITORS AND USE THEREOF
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, (2020/07/14)
The present invention relates to compounds and methods useful for inhibiting the DNA polymerase IIIC enzyme. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of Gram-positive bacterial infections.
IRAK DEGRADERS AND USES THEREOF
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, (2019/07/10)
The present invention provides compounds, compositions thereof, and methods of using the same.
A hit to lead discovery of novel N-methylated imidazolo-, pyrrolo-, and pyrazolo-pyrimidines as potent and selective mTOR inhibitors
Lee, Wendy,Ortwine, Daniel F.,Bergeron, Philippe,Lau, Kevin,Lin, Lichuan,Malek, Shiva,Nonomiya, Jim,Pei, Zhonghua,Robarge, Kirk D.,Schmidt, Stephen,Sideris, Steve,Lyssikatos, Joseph P.
, p. 5097 - 5104 (2013/09/12)
A series of N-7-methyl-imidazolopyrimidine inhibitors of the mTOR kinase have been designed and prepared, based on the hypothesis that the N-7-methyl substituent on imidazolopyrimidine would impart selectivity for mTOR over the related PI3Kα and δ kinases. The corresponding N-Me substituted pyrrolo[3,2-d]pyrimidines and pyrazolo[4,3-d]pyrimidines also show potent mTOR inhibition with selectivity toward both PI3α and δ kinases. The most potent compound synthesized is pyrazolo[4,3-d]pyrimidine 21c. Compound 21c shows a Ki of 2 nM against mTOR inhibition, remarkable selectivity (>2900×) over PI3 kinases, and excellent potency in cell-based assays.
Pyrrolo- and pyrazolo-[3,4-e][1,2,4]triazolo[1,5-c]pyrimidines as adenosine receptor antagonists
Baraldi, Pier Giovanni,Saponaro, Giulia,Aghazadeh Tabrizi, Mojgan,Baraldi, Stefania,Romagnoli, Romeo,Moorman, Allan R.,Varani, Katia,Borea, Pier Andrea,Preti, Delia
experimental part, p. 1046 - 1059 (2012/03/09)
The discovery and development of adenosine receptor antagonists have represented for years an attractive field of research from the perspective of identifying new drugs for the treatment of widespread disorders such as inflammation, asthma and Parkinson's
PYRAZOLEPYRIMIDINE COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE and INFLAMMATORY DISEASES
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Page/Page column 39-40, (2009/07/17)
The present invention relates to compounds that are inhibitors of PDElA, a phosphodiesterase that is involved in the modulation of the degradation of cartilage, joint degeneration and diseases involving such degradation and/or inflammation, and particular
PYRAZOLEPYRIMIDINE COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE and INFLAMMATORY DISEASES
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Page/Page column 48-49, (2009/07/17)
The present invention relates to compounds that are inhibitors of PDElA, a phosphodiesterase that is involved in the modulation of the degradation of cartilage, joint degeneration and diseases involving such degradation and/or inflammation, and particular
Novel compounds useful for the treatment of degenerative and inflammatory diseases
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, (2008/12/07)
The present invention relates to compounds that are inhibitors of PDE1A, a phosphodiesterase that is involved in the modulation of the degradation of cartilage, joint degeneration and diseases involving such degradation and/or inflammation.
SYNTHESES BASED ON DIMETHYLPYRAZOLES. VII. PYRAZOLE ANALOGS OF ANTHRANILIC ACID AND ITS AMIDE. DERIVATIVES OF N-PYRAZOLYLNAPHTHALIMIDES
Perevalov, V. P.,Andreeva, M. A.,Manaev, Yu. A.,Isaev, Sh. G.,Baryshnenkova, L. I.,Stepanov, B. I.
, p. 976 - 980 (2007/10/02)
1-Methyl-4-nitropyrazole-5-carboxylic acid was obtained by the nitration of 1-methylpyrazole-5-carboxylic acid.It was used for the synthesis of 4-amino-1-methylpyrazole-5-carboxylic acid and its amide. 4-Amino-1-methyl-5-carbamoylpyrazole reacts with naphthalic anhydride in acetic acid only at 185-190 deg C with the formation of 1-methyl-1H-pyrazolopyrimidinobenzo-5,13-(5H,13H)isoquinolinedione.The reaction with 4-nitronaphthalic anhydride takes place in acetic acid on boiling.The obtained 2-(5-carbamoyl-1-methyl-4-pyrazolyl)-7-nitrobenzo-1,3-(1H,3H)isoquinolinedione was converted by dehydration in phosphorus oxychloride into the corresponding nitrile and nitrodione.The latter was reduced to the aminodione.The IR and electronic spectra of the dione and nitro- and aminodiones were studied.
